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A series of arylpiperazine derivatives was synthesized to obtain agents sho
wing apparent therapeutic effects in a chronic inflammatory animal model, s
tarting from a lead possessing potent dual cytokine regulatory activity in
vivo. We found a pyrimidylpiperazine derivative 17c showing the dual regula
tory activity and an excellent therapeutic effect in an adjuvant-induced ar
thritis model. (C) 2000 Elsevier Science Ltd. All rights reserved.